US5559102AExpiredUtility
Adenosine and guanosine-3'-5'-cyclic methylphosphonate derivatives
Est. expiryAug 16, 2008(expired)· nominal 20-yr term from priority
C07H 19/20
39
PatentIndex Score
3
Cited by
17
References
26
Claims
Abstract
Cyclic AMP and cyclic GMP derivatives, such as 8-bromoadenosine-3', 5'-cyclic methylphosphonate, are effective in inhibiting phosphodiesterases.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1. A compound of the formula ##STR7## wherein R 1 is hydrogen, hydroxyl or acyloxy; R 2 is lower alkyl; R 3 is hydrogen, methyl or acyl; and R 4 is hydrogen or halo; provided that when R 1 is hydrogen and R 2 is lower alkyl, R 3 and R 4 are not both hydrogen.
2. A compound according to claim 1 wherein R 3 is hydrogen, methyl or acyl of the formula --COR 31 wherein R 31 is lower alkyl or aryl.
3. A compound according to claim 2 wherein R 31 is alkyl of 1 to 4 carbon atoms.
4. A compound according to claim 2 wherein R 31 is phenyl or naphthyl.
5. A compound according to claim 1 wherein R 4 is hydrogen, bromo, chloro or fluoro.
6. A compound according to claim 1 wherein R 6 is hydrogen, bromo, chloro or fluoro.
7. A compound according to claim 1 wherein R 2 is alkyl of 1 to 4 carbon atoms.
8. A pharmaceutical composition which comprises a compound of the formula ##STR8## wherein R 1 is hydrogen, hydroxyl or acyloxy; R 2 is lower alkyl; R 3 is hydrogen, methyl or acyl; and R 4 is hydrogen or halo; provided that when R 1 is hydrogen and R 2 is lower alkyl, R 3 and R 4 are not both hydrogen in combination with a pharmaceutically acceptable carrier.
9. A composition according to claim 8 wherein R 31 is hydrogen, methyl or acyl of the formula --COR 31 wherein R 31 is lower alkyl or aryl.
10. A composition according to claim 9 wherein R 31 is alkyl of 1 to 4 carbon atoms.
11. A composition according to claim 9 wherein R 31 is phenyl or naphthyl.
12. A composition according to claim 8 wherein R 4 is hydrogen, bromo, chloro or fluoro.
13. A pharmaceutical composition which comprises a compound of the formula ##STR9## wherein R 1 is hydrogen, hydroxyl or acyloxy; R 2 is lower alkyl; R5 is hydrogen or acyl and R 6 is hydrogen or halo in combination with a pharmaceutically acceptable carrier.
14. A composition according to claim 13 wherein R 5 is hydrogen or acyl of the formula --COR 51 wherein R 51 is lower alkyl or aryl.
15. A composition according to claim 14 wherein R 51 is alkyl of 1 to 4 carbon atoms.
16. A composition according to claim 14 wherein R 51 is phenyl or naphthyl.
17. A composition according to claim 13 wherein R 6 is hydrogen, bromo, chloro or fluoro.
18. A composition according to claim 8 wherein R 2 is alkyl of 1 to 4 carbon atoms.
19. A compound of the formula ##STR10## wherein R 1 is hydrogen, hydroxyl or acyloxy; R 2 is lower alkyl; R 5 is hydrogen or acyl and R 6 is hydrogen or halo.
20. A compound according to claim 19 wherein R 1 is hydroxyl or acyloxy.
21. A compound according to claim 19 wherein R 2 is alkyl of 1 to 4 carbon atoms.
22. A composition according to claim 13 wherein R 1 is hydroxyl or acyloxy.
23. A composition according to claim 13 wherein R 2 is alkyl of 1 to 4 carbon atoms.
24. A compound according to claim 19 wherein R 5 is hydrogen or acyl of the formula --COR 51 wherein R 51 is lower alkyl or aryl.
25. A compound according to claim 24 wherein R 51 is alkyl of 1 to 4 carbon atoms.
26. A compound according to claim 24 wherein R 51 is phenyl or naphthyl.Cited by (0)
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